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Synthesis and biological evaluation of peptide-siRNA conjugates with phosphodiester unit as linker
Wang XiaoFeng1; Huang Ye1; Liu Yang1,2; Chen Yue1; Jin HongWei1; Zheng Yi1; Du Quan1; Yang ZhenJun1; Zhang LiHe1
关键词siRNA peptide conjugate solid synthesis
刊名SCIENCE CHINA-CHEMISTRY
2013-11-01
DOI10.1007/s11426-013-4912-y
56期:11页:1542-1549
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary
资助者National Natural Science Foundation of China ; Ministry of Science and Technology of China ; National Key Basic Research Program of China ; National Natural Science Foundation of China ; Ministry of Science and Technology of China ; National Key Basic Research Program of China
研究领域[WOS]Chemistry
关键词[WOS]CELL-PENETRATING PEPTIDES ; ANTISENSE OLIGONUCLEOTIDE ; RNA-INTERFERENCE ; VEGF SIRNA ; DELIVERY ; VEHICLES ; THERAPEUTICS ; LOCALIZATION ; STRAND
英文摘要

In this paper, a series of peptide-siRNA conjugates with phosphodiester unit as the linker targeting to Cdc2 gene were synthesized by solid phase stepwise strategy. The conjugation of peptides at either 3′-terminus of siCdc2 bring no change to the classical A-form of RNA duplex, but slightly compromise the thermodynamic stability. Peptide conjugation at the 3′-terminus of sense strand could improve the serum stability obviously, however, the opposite peptide conjugation at the 3′-terminus of antisense strand shows no such influence. According to the results of artificial silencing activity assay system, peptide conjugation at 3′-terminus of antisense strand slightly weakens the silencing activity of siCdc2. But sense strand peptide conjugation exhibits similar silencing activity as native siCdc2, meanwhile, it could mitigate the unwanted off-target effect of sense strand targeting to its own mRNA.

语种英语
所属项目编号20932001 ; 2012AA022501 ; 2012CB720604
资助者National Natural Science Foundation of China ; Ministry of Science and Technology of China ; National Key Basic Research Program of China ; National Natural Science Foundation of China ; Ministry of Science and Technology of China ; National Key Basic Research Program of China
WOS记录号WOS:000326327500008
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60915
专题北京大学药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.CSPC Zhongqi Pharmaceut Technol Shijiazhuang Co L, Shijiazhuang 050035, Peoples R China
推荐引用方式
GB/T 7714
Wang XiaoFeng,Huang Ye,Liu Yang,et al. Synthesis and biological evaluation of peptide-siRNA conjugates with phosphodiester unit as linker[J]. SCIENCE CHINA-CHEMISTRY,2013,56(11):1542-1549.
APA Wang XiaoFeng.,Huang Ye.,Liu Yang.,Chen Yue.,Jin HongWei.,...&Zhang LiHe.(2013).Synthesis and biological evaluation of peptide-siRNA conjugates with phosphodiester unit as linker.SCIENCE CHINA-CHEMISTRY,56(11),1542-1549.
MLA Wang XiaoFeng,et al."Synthesis and biological evaluation of peptide-siRNA conjugates with phosphodiester unit as linker".SCIENCE CHINA-CHEMISTRY 56.11(2013):1542-1549.
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